An inhibitor of menin-MLL interactions
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Isomer(s)
27214MI-3
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MI-2 (hydrochloride)

Item No. 11620

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(4-(5,5-dimethyl-4,5-dihydrothiazol-2-yl)piperazin-1-yl)-6-propylthieno[2,3-d]pyrimidine, dihydrochloride
Molecular Formula
C18H25N5S2 • 2HCl
Formula Weight
448.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 10 mg/mlEthanol: 30 mg/ml
λmax
224, 284 nm
SMILES
CCCC(S1)=CC(C1=NC=N2)=C2N3CCN(C4=NCC(C)(C)S4)CC3.Cl.Cl
InChi Code
InChI=1S/C18H25N5S2.2ClH/c1-4-5-13-10-14-15(20-12-21-16(14)24-13)22-6-8-23(9-7-22)17-19-11-18(2,3)25-17;;/h10,12H,4-9,11H2,1-3H3;2*1H
InChi Key
BJVIQDRKAQVWIM-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $178

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    10 mg

    $242

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    25 mg

    $534

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    Cayman Chemical
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    Product Description

    Menin, a product of the multiple endocrine neoplasia gene, is an essential component of histone methyltransferase complexes involving the mixed lineage leukemia (MLL) gene product.1,2 Also, the leukemogenic activity of MLL fusion proteins depends on their direct interaction with menin.3 MI-2 potently binds menin, blocks the menin-MLL fusion protein interaction (IC50 = 0.45 μM), and induces apoptosis in cells expressing MLL fusion proteins.3 Its actions can be compared with those of MI-nc (Item No. 11621), a weak inhibitor of the menin MLL interaction (IC50 = 193 μM).3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Chandrasekharappa, S.C., Guru, S.C., Manickam, P., et al. Positional cloning of the gene for multiple endocrine neoplasia-type 1. Science 276(5311), 404-407 (1997).

    2. Guccione, E., Bassi, C., Casadio, F., et al. Methylation of histone H3R2 by PRMT6 and H3K4 by an MLL complex are mutually exclusive. Nature 449(7164), 933-937 (2007).

    3. Grembecka, J., He, S., Shi, A., et al. Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia. Nat. Chem. Biol. 8(3), 277-284 (2012).